Brexpiprazole

Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = 1A and 5-HT2A serotonin, dopamine D2L, and alpha1B-, and alpha2C-adrenergic receptors in CHO cell membranes expressing the human receptors. It acts as a partial agonist of 5-HT1A, D2L, and D3 receptors (EC50s = 0.49, 4.0, and 2.8 nM, respectively) and an antagonist of 5-HT2A, 5-HT2B, as well as alpha1B- and alpha2C-adrenergic receptors (IC50s = 6.5, 14, 0.66, and 63 nM, respectively) in vitro. In vivo, brexpiprazole dose-dependently reduces conditioned avoidance response (CAR) time, inhibits locomoter hyperactivity induced by apomorphine (Cay-16094) and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats. It also reduces apomorphine-induced eye blinking in cynomolgus monkeys. Formulations containing brexpiprazole have been used in the treatment of schizophrenia and major depressive disorder.Formal Name: 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-2(1H)-quinolinone. CAS Number: 913611-97-9. Synonyms: OPC 34712. Molecular Formula: C25H27N3O2S. Formula Weight: 433.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:7): 0.1 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 215 nm. SMILES: O=C1C=CC2=C(C=C(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)C=C2)N1. InChi Code: InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29). InChi Key: ZKIAIYBUSXZPLP-UHFFFAOYSA-N.